PA8547601A1 - Inhibidores de la proteasa del vih, composiciones que los contienen, sus usos farmaceuticos y materiales para su sintesis - Google Patents

Inhibidores de la proteasa del vih, composiciones que los contienen, sus usos farmaceuticos y materiales para su sintesis

Info

Publication number
PA8547601A1
PA8547601A1 PA20028547601A PA8547601A PA8547601A1 PA 8547601 A1 PA8547601 A1 PA 8547601A1 PA 20028547601 A PA20028547601 A PA 20028547601A PA 8547601 A PA8547601 A PA 8547601A PA 8547601 A1 PA8547601 A1 PA 8547601A1
Authority
PA
Panama
Prior art keywords
compounds
hiv protease
pharmaceutical
synthesis
compositions
Prior art date
Application number
PA20028547601A
Other languages
English (en)
Spanish (es)
Inventor
Stacie Canan-Koch
Therese Alexander
Mark Barvian
Gary Bolton
Fredrick Boyer
Benjamin Burke
Tod Holler
Tanya Jewell
Josyula Vara Prasad
David Kucera
Maria LINTON
Jeff Machak
Michael Joseph Melnick
Lennert Mitchell
Sean Murphy
Siegfried Heinz Reich
Donald James Skalitzky
John Tatlock
Michael Varney
Stephen Webber
Stephen Worland
Scott Virgil
Original Assignee
Agouron Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Agouron Pharma filed Critical Agouron Pharma
Publication of PA8547601A1 publication Critical patent/PA8547601A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D277/06—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
PA20028547601A 2001-06-11 2002-06-11 Inhibidores de la proteasa del vih, composiciones que los contienen, sus usos farmaceuticos y materiales para su sintesis PA8547601A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US29746001P 2001-06-11 2001-06-11
US29772901P 2001-06-12 2001-06-12

Publications (1)

Publication Number Publication Date
PA8547601A1 true PA8547601A1 (es) 2003-12-30

Family

ID=26970163

Family Applications (2)

Application Number Title Priority Date Filing Date
PA20028547501A PA8547501A1 (es) 2001-06-11 2002-06-11 Inhibidores de la proteasa del vih, composiciones que los contienen, sus usos farmaceuticos y materiales para su sintesis
PA20028547601A PA8547601A1 (es) 2001-06-11 2002-06-11 Inhibidores de la proteasa del vih, composiciones que los contienen, sus usos farmaceuticos y materiales para su sintesis

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PA20028547501A PA8547501A1 (es) 2001-06-11 2002-06-11 Inhibidores de la proteasa del vih, composiciones que los contienen, sus usos farmaceuticos y materiales para su sintesis

Country Status (27)

Country Link
US (4) US7179918B2 (is)
EP (3) EP1409466A2 (is)
JP (2) JP2005508867A (is)
KR (2) KR20040023616A (is)
CN (2) CN1599729A (is)
AP (2) AP2003002915A0 (is)
AR (2) AR036093A1 (is)
AU (2) AU2002316235A2 (is)
BR (2) BR0210344A (is)
CA (2) CA2450265A1 (is)
EA (2) EA008169B1 (is)
GE (1) GEP20063890B (is)
HN (1) HN2002000136A (is)
HR (2) HRP20031014A2 (is)
IL (2) IL159022A0 (is)
IS (2) IS7049A (is)
MA (2) MA27348A1 (is)
MX (2) MXPA03011397A (is)
NO (2) NO20035488D0 (is)
NZ (2) NZ530023A (is)
OA (2) OA12696A (is)
PA (2) PA8547501A1 (is)
PE (2) PE20040241A1 (is)
PL (1) PL366622A1 (is)
TN (1) TNSN03130A1 (is)
TW (1) TW200538447A (is)
WO (2) WO2002100844A2 (is)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
US7094909B2 (en) 2001-06-11 2006-08-22 Agouron Pharmaceuticals, Inc. HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
US7169932B2 (en) 2001-06-11 2007-01-30 Pfizer Inc. HIV protease inhibitors, compositions containing the same, their pharmaceutical uses, material for their synthesis
JP2006076882A (ja) * 2002-09-13 2006-03-23 Sumitomo Pharmaceut Co Ltd 新規なジペプチド化合物及びその医薬用途
WO2005026114A1 (en) * 2003-09-17 2005-03-24 Pfizer Inc. Hiv protease inhibitors, compositions containing the same and their pharmaceutical uses
JP2007513142A (ja) * 2003-12-04 2007-05-24 ファイザー インコーポレイテッド プロテアーゼ阻害剤として有用な化合物の製造法
EP1692104A1 (en) * 2003-12-04 2006-08-23 Pfizer Inc. Methods of preparing compounds useful as protease inhibitors
AU2004295187A1 (en) * 2003-12-04 2005-06-16 Pfizer Inc. Methods for the preparation of stereoisomerically enriched amines
BRPI0417492A (pt) * 2003-12-09 2007-05-29 Pfizer composições compreendendo um inibidor de protease de hiv
MXPA06008632A (es) * 2004-01-30 2006-09-04 Pfizer Combinaciones terapeuticas.
AU2005216712A1 (en) * 2004-01-30 2005-09-09 Pfizer Inc. Compositions comprising HIV protease inhibitor and cytochrome P450 enzyme activity inhibitor
WO2005121094A1 (en) * 2004-06-09 2005-12-22 Pfizer Limited Piperazine and piperidine derivatives as anti-hiv-agents
EP2707346A1 (en) * 2011-05-13 2014-03-19 Vertex Pharmaceuticals Inc. Process for the preparation of protease inhibitors
CN117736134A (zh) * 2012-01-12 2024-03-22 耶鲁大学 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
CN107428734A (zh) 2015-01-20 2017-12-01 阿尔维纳斯股份有限公司 用于雄激素受体的靶向降解的化合物和方法
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
CA2979070A1 (en) 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
GB201511382D0 (en) 2015-06-29 2015-08-12 Imp Innovations Ltd Novel compounds and their use in therapy
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
KR20180097530A (ko) 2015-11-02 2018-08-31 예일 유니버시티 단백질분해 표적화 키메라 화합물(Proteolysis Targeting Chimera compound) 및 그의 제조 및 사용 방법
EP3512842B1 (en) 2016-09-15 2024-01-17 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
KR102173463B1 (ko) 2016-10-11 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해용 화합물 및 방법
CA3042260C (en) 2016-11-01 2023-10-03 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
BR112019011200B1 (pt) 2016-12-01 2021-12-28 Arvinas Operations, Inc Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
EP3559002A4 (en) 2016-12-23 2021-02-17 Arvinas Operations, Inc. CHEMERICAL MOLECULES TARGETING EGFR PROTEOLYSIS AND RELATED METHODS OF USE
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
JP2020504741A (ja) 2016-12-23 2020-02-13 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． Ｒａｆ（急速進行性線維肉腫）ポリペプチドの標的分解のための化合物および方法
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
WO2018140809A1 (en) 2017-01-26 2018-08-02 Arvinas, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
AU2019249231B2 (en) 2018-04-04 2022-04-21 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
WO2021011913A1 (en) 2019-07-17 2021-01-21 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
CN112574201B (zh) * 2019-09-29 2024-04-19 四川科伦博泰生物医药股份有限公司 芳基胺类化合物、包含其的药物组合物及其制备方法和用途
CN110803996B (zh) * 2019-11-13 2022-01-11 台州市创源工业技术有限公司 一种羟基苄胺的合成方法
CN118638043A (zh) 2019-12-19 2024-09-13 阿尔维纳斯运营股份有限公司 用于雄激素受体的靶向降解的化合物和方法
WO2021176369A1 (en) 2020-03-06 2021-09-10 Pfizer Inc. Methods of inhibiting sars-cov-2 replication and treating coronavirus disease 2019
EP4146642A1 (en) 2020-05-09 2023-03-15 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6418260A (en) * 1987-07-14 1989-01-23 Sanyo Electric Co Transistor
CA2056911C (en) 1990-12-11 1998-09-22 Yuuichi Nagano Hiv protease inhibitors
US6313094B1 (en) 1990-12-11 2001-11-06 Japan Energy Corporation β-amino-α-hydroxycarboxylic acid derivatives and HIV protease inhibitors
IE920414A1 (en) 1991-02-08 1992-08-12 Sankyo Co New beta-amino-alpha-hydroxycarboxylic acids and their use
AU3278293A (en) * 1991-12-20 1993-07-28 Syntex (U.S.A.) Inc. Cyclic amides of 3-amino-2-hydroxy-carboxylic acids as hiv-protease inhibitors
DE69322127T2 (de) 1992-05-13 1999-06-24 Japan Energy Corp., Tokio/Tokyo Verfahren zur Herstellung von Peptidderivaten und ihrer Salze
US5644028A (en) * 1992-05-13 1997-07-01 Japan Energy Corporation Process for producing peptide derivatives and salts therefor
AU662434B2 (en) 1992-08-07 1995-08-31 Sankyo Company Limited Peptides capable of inhibiting the activity of HIV protease, their preparation and their use
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
DE69524527D1 (de) * 1994-10-14 2002-01-24 Japan Energy Corp AIDS-hemmende Arzneizubereitung und Verfahren
JPH08259532A (ja) 1995-03-24 1996-10-08 Japan Energy Corp ペプチド様化合物又はその薬理的に許容される塩
US6222043B1 (en) * 1995-06-30 2001-04-24 Japan Energy Corporation Methods of preparing novel dipeptide compounds or pharmaceutically acceptable salts thereof
CA2179935C (en) 1995-06-30 2010-09-07 Ryohei Kato Novel dipeptide compound or pharmaceutically acceptable salt thereof and medical use thereof
JPH1087489A (ja) 1996-09-13 1998-04-07 Sankyo Co Ltd Ａｈｐｂａ構造含有ジペプチド化合物を有効成分とする医薬
JPH10101654A (ja) 1996-10-02 1998-04-21 Japan Energy Corp 新規なジペプチド化合物又はその薬理的に許容される塩及びその医薬用途
JPH10182601A (ja) 1996-12-27 1998-07-07 Japan Energy Corp 新規なジペプチド化合物又はその薬理的に許容される塩及びその医薬用途
AR012374A1 (es) 1997-04-15 2000-10-18 Smithkline Beecham Corp Inhibidores de proteasas, composiones farmaceuticas y usos para la preparacion de medicamentos.
US6673772B2 (en) 1999-01-14 2004-01-06 Sumitomo Pharmaceuticals Company Limited Dipeptide compounds and their use as antiviral agents
WO2000048466A2 (en) 1999-02-19 2000-08-24 Oklahoma Medical Research Foundation Protease inhibitors that overcome drug resistance
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
WO2003035650A1 (fr) 2001-09-25 2003-05-01 Takeda Chemical Industries, Ltd. Inhibiteur d'entree
JP2003119137A (ja) 2001-10-10 2003-04-23 Japan Tobacco Inc Ｈｉｖ阻害剤
AU2002334205B2 (en) 2001-10-26 2007-07-05 Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
AU2002349675A1 (en) 2001-12-05 2003-06-17 Shionogi And Co., Ltd. Derivative having hiv integrase inhibitory activity
RU2284315C2 (ru) 2001-12-12 2006-09-27 Бристол-Маерс Сквибб Компани Ингибиторы вич-интегразы и содержащие их фармацевтические композиции
DE60315796T2 (de) 2002-01-17 2008-06-05 Merck & Co., Inc. Hydroxynaphthyridinoncarbonsäureamide, die sich als inhibitoren der hiv-integrase eignen
TW200306192A (en) 2002-01-18 2003-11-16 Bristol Myers Squibb Co Tricyclic 2-pyrimidone compounds useful as HIV reverse transcriptase inhibitors
WO2005026114A1 (en) * 2003-09-17 2005-03-24 Pfizer Inc. Hiv protease inhibitors, compositions containing the same and their pharmaceutical uses
EP1692104A1 (en) * 2003-12-04 2006-08-23 Pfizer Inc. Methods of preparing compounds useful as protease inhibitors

Also Published As

Publication number Publication date
MXPA03011397A (es) 2005-03-07
AU2002345644A2 (en) 2002-12-23
OA12697A (en) 2006-06-21
MA27348A1 (fr) 2005-06-01
NZ530023A (en) 2005-10-28
IL159022A0 (en) 2004-05-12
KR20040035601A (ko) 2004-04-29
CA2450265A1 (en) 2002-12-19
NZ530024A (en) 2005-10-28
CN1622942A (zh) 2005-06-01
BR0210344A (pt) 2004-07-13
WO2002100844A2 (en) 2002-12-19
WO2002100845A8 (en) 2003-03-20
US6953858B2 (en) 2005-10-11
JP2004534061A (ja) 2004-11-11
HRP20031014A2 (en) 2005-10-31
PE20040479A1 (es) 2004-09-20
CN100338044C (zh) 2007-09-19
PL366622A1 (en) 2005-02-07
HRP20031015A2 (en) 2005-10-31
AP2003002915A0 (en) 2003-12-31
AP1770A (en) 2007-08-22
EP1739082A1 (en) 2007-01-03
US20030153507A1 (en) 2003-08-14
PE20040241A1 (es) 2004-04-26
US20050250707A1 (en) 2005-11-10
AU2002345644B2 (en) 2006-08-10
OA12696A (en) 2006-06-22
GEP20063890B (en) 2006-08-10
JP2005508867A (ja) 2005-04-07
US7179918B2 (en) 2007-02-20
BR0210358A (pt) 2004-06-22
TNSN03130A1 (en) 2005-12-23
CA2450269A1 (en) 2002-12-19
IS7050A (is) 2003-11-21
EP1409466A2 (en) 2004-04-21
IS7049A (is) 2003-11-21
NO20035488D0 (no) 2003-12-10
MA27347A1 (fr) 2005-06-01
NO20035489D0 (no) 2003-12-10
AP2003002916A0 (en) 2003-12-31
AU2002345644C1 (en) 2002-12-23
PA8547501A1 (es) 2003-02-14
EA200400026A1 (ru) 2004-04-29
MXPA03011336A (es) 2004-12-06
WO2002100844A3 (en) 2003-03-06
TW200538447A (en) 2005-12-01
US20030225071A1 (en) 2003-12-04
AR036093A1 (es) 2004-08-11
HN2002000136A (es) 2003-07-31
IL159076A0 (en) 2004-05-12
WO2002100845A1 (en) 2002-12-19
AU2002316235A2 (en) 2002-12-23
EA008169B1 (ru) 2007-04-27
AR036046A1 (es) 2004-08-04
EP1448539A1 (en) 2004-08-25
EA200400023A1 (ru) 2004-06-24
CN1599729A (zh) 2005-03-23
US20070021354A1 (en) 2007-01-25
KR20040023616A (ko) 2004-03-18

Similar Documents

Publication Publication Date Title
PA8547601A1 (es) Inhibidores de la proteasa del vih, composiciones que los contienen, sus usos farmaceuticos y materiales para su sintesis
PE20181045A1 (es) Compuestos utiles como inmunomoduladores
GT200100014A (es) Compuestos de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo.
ES2181725T3 (es) Inhibidores de hiv proteasa.
UY29458A1 (es) Heterociclos sustituidos y usos de los mismos
AR030540A1 (es) Compuestos antipicornavirales y composiciones, su uso farmaceutico, y materiales para su sintesis
CO5271715A1 (es) 7-aza-indolin-2-onas sustituidas en 4 y su uso como inhibidores de proteiuna quinasa
UY27882A1 (es) Compuestos quimicos
BRPI0415613A (pt) novos compostos de diazaspiroalcanos e seu uso no tratamento de doenças mediadas por ccr8
CR7716A (es) Uso de inhibidores de la ikb-quinasa para el tratamiento del dolor
UY29869A1 (es) Compuestos de benzamida
BR9708114A (pt) Análogos xantona para o tratamento de doenças infecciosas.
CL2004000590A1 (es) Compuestos derivados de 1,3,4-oxadiazol-3-ona, 1,3,4-tiadiazol-2-ona y de 1,2,4-triazol-3-ona; composicion farmaceutica que los contiene; procedimiento de preparacion y su uso en la preparacion de un medicamento en los que esta relacionado el virus v
UY27851A1 (es) Difenilazetidinonas sustituidas en anillo, procedimiento para su preparacion, medicamentos que comprenden estos compuestos y su uso.
ECSP045477A (es) COMPUESTOS DE AMIDAS DE ÁCIDO3-AMINO-TIENO[2,3-b]PIRIDINO-2-CARBOXÍLICO SUSTITUIDOY PROCEDIMIENTOS PARA PREPARARLOS Y SUS USOS.
UY26666A1 (es) Compuestos y composiciones antipicornavirales, sus usos farmaceuticos y los materiales para su sintesis
CL2023002074A1 (es) Compuestos de piridotriazina sustituidos y usos de estos
UY26877A1 (es) Compuestos pirazol-tiazol, composiciones farmacéuticas que los contienen, y su modo de empleo para inhibir quinasas ciclino- dependientes
ATE432936T1 (de) Imidazotriazin verbindungen zur behandlung von krebserkrankungen
UY27394A1 (es) Pedidos con actividad anti- angiogéna.
SV2004001577A (es) Inhibidores de la hiv proteasa, composiciones que los contienen, sus usos farmacéuticos y materiales para su síntesis
ECSP034892A (es) Inhibidores de proteasa vih, composiciones que los contienen, sus usos farmaceuticos y materiales para su síntesis
DOP2002000415A (es) Inhibidores dela proteasa del vih, composociones conteniendo los mismos, sus usos farmaceuticos y materiales para su sintesis.
UY27331A1 (es) Inhibidores de la proteasa del vih, composiciones que los contienen, sus usos farmacéuticos y materiales para su síntesis
SV2004001553A (es) Proteasa inhibidora de vih, composiciones que las contienen, sus usos farmaceuticos y materiales para su sintesis